Drug intelligence / Profile preview

pregabalin + oxcarbazepine

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Pregabalin + oxcarbazepine is a combination of two antiepileptic (anticonvulsant) drugs used together primarily for the management of partial-onset seizures and potentially for neuropathic pain. Pregabalin is a structural analogue of gamma-aminobutyric acid (GABA) that binds to the alpha-2-delta subunit of voltage-gated calcium channels in the central nervous system, reducing neurotransmitter release and neuronal excitability. Oxcarbazepine is a prodrug that is converted to its active metabolite, which blocks voltage-sensitive sodium channels, stabilizing hyperexcited neural membranes and inhibiting repetitive neuronal firing. The combination may provide additive anticonvulsant effects; preclinical studies show additive or synergistic interactions in seizure models without significant acute adverse effects on motor coordination or memory. However, combined use can increase risks of central nervous system depression such as dizziness, drowsiness, confusion, and impaired concentration[1][2][3][4].

02

Targets

CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)NaV (Voltage-gated sodium channels)

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